CHR-6494

• CAT Number: I001272
• CAS Number: 1333377-65-3
• Molecular Formula: C16H16N6
• Molecular Weight: 292.3
• Purity: ≥95%
• Target: Haspin
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: N/A
• InChIKey: CZZCAOGIEGXMBZ-UHFFFAOYSA-N

CHR-6494 is a potent and selective Haspin (Haploid Germ Cell-Specific Nuclear Protein Kinase) inhibitor that blocks H3T3ph phosphorylation.IC50 Value: N/ATarget: Haspin KinaseCHR-6494 is a first-in-class Haspin inhibitor with a wide spectrum of anticancer effects. Recent research showed that CHR-6494 reduces H3T3ph levels in a dose-dependent manner and causes a mitotic catastrophe characterized by metaphase misalignment, spindle abnormalities and centrosome amplification. From the cellular standpoint, the identified small-molecule Haspin inhibitor causes arrest in G2/M and subsequently apoptosis. Importantly, ex vivo assays also demonstrate its anti-angiogenetic features; in vivo, it shows antitumor potential in xenografted nude mice without any observed toxicity.

Reference

[1]. Cuny, Gregory D.; Ulyanova, Natalia P.; Patnaik, Debasis et al. Structure-activity relationship study of beta-carboline derivatives as haspin kinase inhibitors. Bioorganic & Medicinal Chemistry Letters (2012), 22(5), 2015-2019.
[2]. Huertas, D.; Soler, M.; Moreto, J. et al. Antitumor activity of a small-molecule inhibitor of the histone kinase Haspin. Oncogene (2012), 31(11), 1408-1418.
[3]. Wang F, Ulyanova NP, Daum JR et al. Haspin inhibitors reveal centromeric functions of Aurora B in chromosome segregation. J Cell Biol. 2012 Oct 15;199(2):251-68.